Fibroblast Growth Factor Receptor (FGFR)

<p>Pazopanib (GW786034) is an inhibitor of protein tyrosine kinases that inhibits VEGFR1/2/3. Pazopanib has antitumor activity. Cost-effective and quality-assured.</p>

<p>Lenvatinib (E7080) is a multi-target receptor tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, KIT, PDGFR, and RET, and has oral activity.</p>

<p>Formononetin (Flavosil) is an O-methylated isoflavone and a phytoestrogen from the root of Astragalus membranaceus.</p>

<p>2,5-Dihydroxybenzoic acid (Gentisic acid) is an active metabolite of salicylic acid degradation with a broad spectrum of biological activity.</p>

<p>FGFR1/DDR2 inhibitor 1 is an inhibitor of discoindin domain receptor 2 (DDR2) and fibroblast growth factor receptor 1 (FGFR1), with IC50 values of 31.1 nM, 108</p>

<p>Pemigatinib (INCB054828) is an orally active, selective inhibitor of FGFR(IC50s of 0.4 nM, 0.5 nM, 1.2 nM, 30 nM for FGFR1, FGFR2, FGFR3, FGFR4, respectively).</p>

<p>Aprutumab, a human FGFR2 monoclonal antibody, targets FGFR2-IIIB/C and is used in antibody-drug conjugates.</p>

<p>Triamcinolone acetonide (Azmacort) is a Corticosteroid.</p>

<p>Ferulic Acid (Coniferic acid) is a highly abundant phenolic phytochemical and a organic compound found in the Ferula assafoetida L. or Ligusticum chuanxiong.</p>

<p>Lucitanib (E-3810) is a VEGFR/FGFR inhibitor targeting VEGFR1-3 and FGFR1-2 with IC50s 7-82.5 nM.</p>

<p>Mal-amido-PEG2-C2-amido-Ph-C2-CO-AZD (PF-05231023) is a long-acting fibroblast growth factor 21 (FGF21) analog and is an FGF21-receptor agonist.</p>

<p>LC-MB12 is a PROTAC FGFR2 compound that degrades FGFR2 and can be used to study gastric cancer.</p>

<p>Bemarituzumab: humanized IgG1 antibody inhibits FGFR2b, may be used in cancer research.</p>

<p>Si5-N14 is a key component of siloxane-linked lipid nanoparticles (SiLNP) with properties that enhance vascular repair and exhibit antitumor activity. In transgenic GFP mouse models, Si5-N14 mediates CRISPR-Cas9 editing. In Lewis lung carcinoma (LLC) tumor mouse models, it leads to the knockdown of vascular endothelial growth factor receptor 2 (VEGFR2), producing antitumor effects. Additionally, in mice with virus-induced lung injury, Si5-N14 facilitates the delivery of fibroblast growth factor-2 (FGF-2) mRNA, promoting vascular repair, oxygenation, and improved lung function. Si5-N14 shows potential for research in tumors, pneumonia, and cardiovascular diseases.</p>

<p>S6K2-IN-1 (Compound 2) is an inhibitor of S6K2 with an IC50 of 22 nM and also exhibits inhibitory activity against FGFR4 with an IC50 of 216 nM.</p>

<p>E-7090 is a fibroblast growth factor receptor inhibitor. E-7090 is a selective inhibitor of the tyrosine kinase activities of FGFR1, -2, and -3.</p>

<p>A unique collection of 1016 tyrosine kinase inhibitors for high throughput screening and high content screening for drug discovery in tyrosine kinase related</p>

<p>Vofatamab (B-701) is a fully human monoclonal antibody targeting FGFR3, often used in combination with other compounds to treat cancer.</p>

<p>FGFR4-IN-14 (Compound 27i) is a selective FGFR4 inhibitor with an IC50 of 2.4 nM, showing potent inhibition of cell proliferation in the V550L and N535K mutant</p>

<p>Efimosfermin alfa is a humanized antibody targeting FGFR1.</p>

<p>Fazpilodemab (BFKB8488A) is a humanized bispecific antibody that targets and activates the Klotho β and fibroblast growth factor receptor 1c receptor complex.</p>

<p>FGFR1 inhibitor-8 (Compound 9), an FGFR1 inhibitor with an IC50 of 0.5 nM, binds to the ATP-binding pocket of FGFR1 and exhibits anticancer activity [1].</p>

<p>FGFR1 inhibitor-9 (Compound 7) is an FGFR1 inhibitor with potent binding affinity, exhibiting an IC50 of 0.85 nM.</p>

<p>U3-1784 is a humanized monoclonal antibody targeting CD334, with anti-cancer activity, used in liver cancer research.</p>

<p>IMC-D11 (LY-3076226 antibody) is an IgG1 monoclonal antibody targeting FGFR3. It serves as the antibody component of LY3076226. For its isotype control, refer to Human IgG1 kappa, Isotype Control.</p>

<p>PKCε (85-92) (ψεRACK) is a peptide and selective PKCε activator, induces a pro-angiogenic response, promotes FGF-2 cytosolization, regulates VEGF activity.</p>

<p>FGFR1/VEGFR2-IN-1 (compound 2b) is an inhibitor of both FGFR1 and VEGFR2, applicable in cancer research [1].</p>

<p>BW710 is an orally active inhibitor specifically targeting fibroblast growth factor receptor 2 (FGFR2). It effectively inhibits the proliferation of BaF3-FGFR2 cells with an IC50 value of 2.8 nM. BW710 completely suppresses FGFR2 enzymatic activity and demonstrates selectivity among 75 tyrosine kinases, including FGFR1, FGFR3, and FGFR4, at a 1 μM concentration. Additionally, BW710 impedes FGFR2 signaling and selectively inhibits the proliferation of cancer cells driven by FGFR2. It exhibits promising pharmacokinetic properties, with an oral bioavailability of 29% in mice.</p>

<p>FGFR1 inhibitor-2, potent at 4.55 μM IC50 in MDA-MB-231, targets triple-negative breast cancer.</p>

<p>Recifercept (TA-46) is a recombinant human soluble fibroblast growth factor receptor 3, a decoy protein that competes for ligands of mutant FGFR3.</p>

<p>FGFR2 degrader1 (compound 28E) is a selective PROTACS degrader of FGFR2, with a DC50 of 0.645 nM. FGFR2 plays a significant role in cancer research.</p>

<p>Arg-IN-1 is a selective covalent inhibitor targeting Arginine (Arg), with IC50 values of 9.7 nM and 30.4 nM for FGFR2 and FGFR3, respectively. This compound is designed to potentially avoid the off-target toxicity of FGFR1/4 and overcome acquired resistance, offering potential in cancer therapies targeting FGFR.</p>

<p>FGFR1 Inhibitor 7 (compound 5), a potent FGFR1 tyrosine kinase inhibitor, exhibits an IC50 of 0.33 nM against its target and demonstrates broad-spectrum</p>

<p>Efruxifermin, a modified FGF21 with IgG1 Fc, has increased stability and affinity. Used in non-alcoholic steatohepatitis research.</p>

<p>Gunagratinib (ICP-192) is a pan-FGFR inhibitor, useful in research on FGFR-related diseases.</p>

<p>PROTAC FGFR1 degrader-1 (compound S2H) is a targeted degrader of FGFR1, demonstrating an IC50 of 26.81 nM and a DC50 of 39.78 nM in KG1a cells. This compound is composed of a CRBN-type E3 ligase ligand (blue part) Pomalidomide, a target protein ligand (red part) FGFR1ligand-1, and a PROTAC linker (black part) 9-Bromononanoic acid, together forming the conjugate E3LigaseLigand-linker Conjugate 164.</p>

<p>NSC 12 is an orally active pan-FGF trap that binds FGF2 and interferes with its interaction with FGFR1 with potential FGF-dependent antitumor activity.</p>

<p>SM27 is a fibroblast growth factor 2 (FGF2) inhibitor with anti-angiogenic activity and can be used to study tumours.</p>

<p>(Z)-Orantinib, oral ATP-competitive blocker for Flk-1/KDR, PDGFRβ, FGFR1 (IC50: 2.1, 0.008, 1.2 μM), is a strong antiangiogenic, antitumor drug.</p>

<p>FIIN-3 is an irreversible inhibitor of FGFR.</p>

<p>Masitinib (AB1010) is a tyrosine-kinase inhibitor used in the treatment of mast cell tumors in animals, specifically dogs.</p>

<p>Dovitinib lactate (TKI-258 lactate)(TKI258) lactate is a potent inhibitor of fibroblast growth factor receptor 3 (FGFR3) (IC50 :5 nM).</p>

<p>PRN1371 is a specific and potent FGFR1-4 and CSF1R inhibitor (IC50s: 0.6/1.3/4.1/19.3/8.1 nM for FGFR1/2/3/4 and CSF1R).</p>

<p>SU4984 is a cell-permeable, ATP-competitive and reversible inhibitor of the fibroblast growth factor receptor 1 (FGFR1).</p>